Voltage-gated ion channels are important targets for therapeutic intervention. Defects in voltage-gated ion channel function are linked to numerous biological outcomes, including, but not limited to cardiovascular, metabolic, and autoimmune disorders, pain and neurological disorders, and cancer. The identification of molecules that modulate the activity of voltage-gated proteins (hereafter, “VGPs”) is difficult and relatively non-specific. There is a demand for screening methods suitable for identifying molecules that bind specifically to particular VGPs functional regions and for identifying molecules that bind specifically to particular VGP functional/conformational states. This invention addresses these needs.